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Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers

Asian Pacific Journal of Tropical Medicine 2019年第5期12卷 195-203页

作者： Kabita Gogoi Gokul Baishya Biswajit Saikia Nabin Chandra Barua Chandrajit Dohutia Akalesh Kumar Verma Anil Prakash ICMR-Regional Medical Research Centre N.E. CSIR-North-East Institute of Science and Technology digboi college Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University Zoology Department ICMR-National Institute for Research in Environmental Health

Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial ***: Three different reaction schemes were used to synthesize a total of 15 artemisininbased *** first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of *** second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired ***-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound *** potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous *** third scheme involved the Huisgen 1,3-dipolar cycloaddition between the synthesized aliphatic and aromatic diazides and two alkyne derivatives of artemisinin to obtain the desired artemisinin dimers with average ***: The best in vitro antiplasmodial activity was shown by the compound GB-2 registering IC_(50) value 0.066 μg/mL against chloroquine-sensitive and 0.865 μg/mL against chloroquineresistant strains of Plasmodium *** suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight *** docking interactions of Plasmodium falciparum ATP6(PfATP6) protein revealed strong bonding of GB-2 with Thr255 residue which is likely to be the reason for excellent antimalarial activity of this ***: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial *** the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking *** helped in identifying artemisinin analogues possessing good antimalarial properties a

关键词： Antimalarial activity Artemisinin derivatives Huisgen reaction Triazole dimers Plasmodium berghei Plasmodium falciparum Molecular docking

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Localization of polycyclic aromatic hydrocarbons and heavy metals in surface soil of Asia’s oldest oil and gas drilling site in Assam,northeast India:Implications for the bio-economy

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Emerging Contaminants 2016年第3期2卷 119-127页

作者： Hemen Sarma N.F.Islam P.Borgohain A.Sarma M.N.V.Prasad Department of Botany N N Saikia CollegeTitabarAssamIndia Department of Biotechnology Pandu CollegeGuwahatiAssamIndia Department of Plant Science University of HyderabadHyderabadTelanganaIndia

The environmental influx of hazardous contaminants viz PAHs and HMs occurs due to oil and gas drilling,and processing of petroleum products in industrial facilities and *** problem plagues crude oil drilling sites as PAHs are an essential component of and HMs coexist with crude *** analyzed the spatial distribution of 16 PAHs and 8 HMs in 10 contaminated sites of Assam,a state in *** included digboi,where crude oil was drilled in 1867 and the first oil well in Asia that was ***Ʃ16 PAHs in soil were detected with a minimum of 13.48 and a maximum of 86.3 mgkg1 andƩ8 heavy metal concentrations in the soil ranged between 69.51 and 336.06 mgkg1.A negative correlation was detected between the relative concentrations of PAHs and *** results confirmed that the nonbiodegradable nature of HMs made them stay in the soil for longer periods of *** our study,we found that the levels of lead,copper,nickel,and chromium(total)in soil were 73.62,11.86,58.97 and 158.66 mgkg*** recovery percentage for PAHs and HMs were in the range of 67e97%and 90e95%*** distribution indices for Phenanthrene/Anthracene,Naphthalene/Acenapthhylene,Chyrsene/Benzo(g,h,i)perylene and Fluranthene/Pyrene)calculated for soil samples indicated that the spatial distribution of PAHs in soil is uneven which might be due to variations in contaminates disseminated in *** regionalized concentration has serious implications on the bio-economy both in terms of health and economy,especially since the proximity of crude oil sites to paddy fields and/or tea plantations uniquely marks the landscape of upper Assam.

关键词： PAH Heavy metals Spatial distribution indices Oil Drilling site

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